WO2012041263A3 - Procédé de fabrication d'une 2-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phényl]- l,3-oxazolidin-5-yl}méthyl)-lh-isoindol-l,3(2h)-dione à la pureté optique élevée - Google Patents

Procédé de fabrication d'une 2-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phényl]- l,3-oxazolidin-5-yl}méthyl)-lh-isoindol-l,3(2h)-dione à la pureté optique élevée Download PDF

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Publication number
WO2012041263A3
WO2012041263A3 PCT/CZ2011/000095 CZ2011000095W WO2012041263A3 WO 2012041263 A3 WO2012041263 A3 WO 2012041263A3 CZ 2011000095 W CZ2011000095 W CZ 2011000095W WO 2012041263 A3 WO2012041263 A3 WO 2012041263A3
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WO
WIPO (PCT)
Prior art keywords
oxo
isoindol
dione
phenyl
oxazolidin
Prior art date
Application number
PCT/CZ2011/000095
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English (en)
Other versions
WO2012041263A2 (fr
Inventor
Miroslav Urbasek
Pavel Hradil
Martin Grepl
Petra Fialova
Vladimir Oremus
Petr Slezar
Original Assignee
Farmak, A.S.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Farmak, A.S. filed Critical Farmak, A.S.
Publication of WO2012041263A2 publication Critical patent/WO2012041263A2/fr
Publication of WO2012041263A3 publication Critical patent/WO2012041263A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La présente invention concerne une 2-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phényl]-l,3-oxazolidin- 5-yl} méthyl)- lH-isoindol- l,3(2H)-dione (I) très pure optiquement obtenue par réaction d'une 2-((2R)-2-hydroxy-3-[4-(3- oxo-4-morpholinyl)phényl]amino-propyl)- lH-isoindol- l,3(2H)-dione (III), contenant l'isomère (2S) (IIIb), avec N,N-carbonyldiimidazole dans du tétrahydrofuranne, de préférence sans la présence du catalyseur 4-diméthylaminopyridine, ladite réaction étant menée de façon à ce qu'elle soit terminée au moment où le mélange réactionnel contient encore le composé n'ayant pas réagi de formule III en quantité allant de 3 à 5 fois la quantité initiale de l'isomère (2S) dans la substance de départ de formule III.
PCT/CZ2011/000095 2010-09-30 2011-09-27 Procédé de fabrication d'une 2-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phényl]- l,3-oxazolidin-5-yl}méthyl)-lh-isoindol-l,3(2h)-dione à la pureté optique élevée WO2012041263A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CZPV2010-714 2010-09-30
CZ20100714A CZ2010714A3 (cs) 2010-09-30 2010-09-30 Zpusob výroby 2-({(5S)-2-oxo-3-[4-(3-oxo-4-morfolinyl)fenyl]-1,3oxazolidin-5-yl}methyl)-1H-isoindol-1,3(2H)-dionu ve vysoké optické cistote

Publications (2)

Publication Number Publication Date
WO2012041263A2 WO2012041263A2 (fr) 2012-04-05
WO2012041263A3 true WO2012041263A3 (fr) 2012-06-21

Family

ID=45418269

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CZ2011/000095 WO2012041263A2 (fr) 2010-09-30 2011-09-27 Procédé de fabrication d'une 2-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phényl]- l,3-oxazolidin-5-yl}méthyl)-lh-isoindol-l,3(2h)-dione à la pureté optique élevée

Country Status (2)

Country Link
CZ (1) CZ2010714A3 (fr)
WO (1) WO2012041263A2 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE037188T2 (hu) 2012-12-21 2018-08-28 Farma Grs D O O Eljárás rivaroxaban elõállítására
WO2016030669A1 (fr) * 2014-08-25 2016-03-03 Cipla Limited Procédé de préparation du rivaroxaban
CN110054623A (zh) * 2019-05-29 2019-07-26 浙江燎原药业股份有限公司 一种利伐沙班中间体的制备方法
CN111675705A (zh) * 2020-08-11 2020-09-18 北京鑫开元医药科技有限公司 一种4-(4-氨基苯基)吗啉-3-酮衍生物的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001047919A1 (fr) * 1999-12-24 2001-07-05 Bayer Aktiengesellschaft Oxazolidinones substituees et leur utilisation dans le domaine de la coagulation sanguine
DE102004002044A1 (de) * 2004-01-15 2005-08-04 Bayer Healthcare Ag Herstellverfahren

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2425183T3 (es) 2007-08-14 2013-10-11 Concert Pharmaceuticals Inc. Derivados de oxazolidinonas sustituidas

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001047919A1 (fr) * 1999-12-24 2001-07-05 Bayer Aktiengesellschaft Oxazolidinones substituees et leur utilisation dans le domaine de la coagulation sanguine
DE102004002044A1 (de) * 2004-01-15 2005-08-04 Bayer Healthcare Ag Herstellverfahren

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DISCLOSED ANONYMOUSLY: "Crystalline form of 2-({2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)-1H-isoindole-1,3(2H-dione", IP.COM JOURNAL, vol. 10(6A), no. 17 (ipcom000195959D), 24 May 2010 (2010-05-24), XP002674230, ISSN: 1533-0001 *

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Publication number Publication date
WO2012041263A2 (fr) 2012-04-05
CZ2010714A3 (cs) 2012-04-11

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